| 2β-(4′-甲基- 1′-哌嗪基)- 3α-羟基-16,17-取代-5α-雄甾烷的合成 |
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| 引用本文： | 何群,徐有恒.2β-(4′-甲基- 1′-哌嗪基)- 3α-羟基-16,17-取代-5α-雄甾烷的合成[J].药学学报,1992,27(2):101-106. |
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| 作者姓名： | 何群 徐有恒 |
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| 作者单位： | 湖南医科大学血液生理研究室,长沙410078 |
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| 摘 要： | 为了寻找心血管系统药物,以表雄酮为原料,合成了7个16,17位取代的目标化合物:2β-(4’-甲基-1’-哌嗪基)-3α-羟基-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α-羟基-16α-溴-5α-雄甾-17-酮、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-氧-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17-肟-5α-雄甾烷、2β-(4’-甲基-1’-哌嗪基)-3α,16α-二羟基-17β-氨基-5α-雄甾烷和2β—(4’-甲基-1’-哌嗪基)-3α,17β-二羟基-16β-氨基-5α-雄甾烷。初步药理试验结果表明它们都有不同程度的抗心律失常活性。
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| 关 键 词： | 表雄酮 邻氨基醇-5α-雄甾烷 抗心律失常药 |
| 收稿时间： | 1991-01-03 |
Synthesis of 2 beta-(4'-methyl-1'-piperazino)-3 alpha-hydroxyl-16,17- substituted-5 alpha-androstanes] |
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| Q He,YH Xu.Synthesis of 2 beta-(4''-methyl-1''-piperazino)-3 alpha-hydroxyl-16,17- substituted-5 alpha-androstanes][J].Acta Pharmaceutica Sinica,1992,27(2):101-106. |
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| Authors: | Q He YH Xu |
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| Institution: | Research Laboratory of Blood Physiology, Human Medical University, Changsha. |
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| Abstract: | According to some studies, the vicinal amino-alcohol compounds of 5 alpha-androstane possess to a certain extent biological activities in cardiovascular system. In order to find new antiarrhythmic agents, seven new 2 beta-(4'-methyl-1'-piperazino)-3 alpha-hydroxyl-16, 17-substituted-5 alpha-androstanes were synthesized through 2 alpha,3 alpha-epoxyl-5 alpha-adrostan-17-one from epiandrosterone. Preliminary results of biological experiment showed that they possess to a different extent antiarrhythmic activities among which compounds VI, XI and XIV showed higher activities than others. |
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| Keywords: | Vicinal aminoalcohol-5α-androstane antiarrhythmic agent Epiandrosterone |
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